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Roxatidine Acetate Hydrochloride


Drug Approvals

(BANM, US Adopted Name, rINNM)

Synonyms: Hoe-062 (roxatidine); Hoe-760; Pifatidine Hydrochloride; Roxatidina, hidrocloruro de acetato de; TZU-0460
BAN: Roxatidine Acetate Hydrochloride [BANM]
USAN: Roxatidine Acetate Hydrochloride
INN: Roxatidine Acetate Hydrochloride [rINNM (en)]
INN: Hidrocloruro de acetato de roxatidina [rINNM (es)]
INN: Roxatidine, Acétate de [rINNM (fr)]
INN: Roxatidini Acetas [rINNM (la)]
INN: Роксатидина Ацетат [rINNM (ru)]
Chemical name: N-{3-[(α-Piperidino-m-tolyl)oxy]propyl}glycolamide acetate monohydrochloride
Molecular formula: C17H26N2O3,C2H2O,HCl =384.9
CAS: 78273-80-0 (roxatidine); 97900-88-4 (roxatidine hydrochloride); 78628-28-1 (roxatidine acetate); 93793-83-0 (roxatidine acetate hydrochloride)
ATC code: A02BA06

Pharmacopoeias. In Japan.

Stability. The stability of roxatidine acetate hydrochloride in parenteral nutrition solutions was influenced by storage temperature and amino acid content and composition.

Adverse Effects and Precautions

As for Cimetidine.

Interactions

Unlike cimetidine roxatidine does not appear to affect cytochrome P450, and therefore is considered to have little effect on the metabolism of other drugs. However, like other H2-antagonists its effects on gastric pH may alter the absorption of some other drugs.

Pharmacokinetics

Roxatidine acetate hydrochloride is rapidly and almost completely absorbed from the gastrointestinal tract with peak concentrations in plasma occurring about 1 to 3 hours after doses by mouth. It is rapidly hydrolysed to the active desacetyl metabolite, roxatidine, by esterases in the liver, small intestine, and serum. Over 90% of a dose is excreted in the urine as roxatidine and other metabolites. The elimination half-life of roxatidine is about 6 hours and is prolonged in renal impairment. Small amounts of roxatidine have been reported to be distributed into breast milk.

Uses and Administration

Roxatidine acetate hydrochloride is an H2-antagonist with actions and uses similar to those of cimetidine. In the management of peptic ulcer disease the oral dose is 150 mg at bedtime or 75 mg twice daily for 4 to 6 weeks. Where appropriate a maintenance dose of 75 mg at bedtime may be given to prevent the recurrence of ulcers. In gastro-oesophageal reflux disease the recommended dose is 150 mg at bedtime or 75 mg twice daily for 6 to 8 weeks. Gastritis has been managed with 75 mg once daily in the evening, and a dose of 75 mg twice daily has been used for Zollinger-Ellison syndrome.

When used as a pre-anaesthetic medication, an oral dose of roxatidine acetate hydrochloride 75 mg is given in the evening on the day before surgery and repeated 2 hours before the induction of anaesthesia alternatively a single dose of 150 mg may be given the night before surgery.

Roxatidine acetate hydrochloride may also be given intravenously for the treatment of upper gastrointestinal tract haemorrhage in a dose of 75 mg twice daily by slow intravenous injection or by intravenous infusion. For dosage in renal impairment, see below.

Administration in renal impairment. The dosage of roxatidine acetate hydrochloride should be reduced in patients with renal impairment. Suggested oral doses, based on creatinine clearance (CC), for patients on acute therapy are:

• CC 20 to 50 mL/minute: 75 mg at bedtime

• CC less than 20 mL/minute: 75 mg every 2 days.

However, results in 6 patients with chronic renal failure and CC less than 20 mL/minute indicated that giving the recommended dose of roxatidine acetate hydrochloride, 75 mg every other day, was inadequate to maintain gastric pH above 4 for more than 6 hours. Subsequent study in 8 patients showed that a dose of 75 mg daily was well tolerated and effective.

Proprietary Preparations

Germany: Roxit

Greece: Roxanel

India: Rotane

Italy: Gastralgin; Neo H2; Roxit

Japan: Altat

The Netherlands: Roxit

South Africa: Roxit

Spain: Roxiwas; Zarocs

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